A set of 1-(arylalkyl)quinolizidines, isosteric thio analogs, and variously functionalized congeners were synthesized and tested for affinity to sigma1 and sigma2 receptor subtypes, by displacing [3H]-(+)-pentazocine and [3H]DTG from guinea pig brain and rat brain prepns., resp. All compds. exhibited a good affinity for the sigma1 subtype, with subnanomolar Ki values for the best of them, while only modest or poor affinity for the sigma2 subtype was obsd. Some structure-activity relationships were put forward.
|Titolo:||1-(arylalkyl)quinolizidine derivatives and thio-isosteric analogs as ligands for sigma receptors|
|Autori interni:||SPARATORE, ANNA CONCETTINA (Corresponding)|
|Parole Chiave:||tumor-cell-lines; pharmacological evaluation; quinolizidine derivatives; selective sigma(1); grignard reagents; binding; sterochemistry; potent; thiolupinine; affinity|
|Settore Scientifico Disciplinare:||Settore CHIM/08 - Chimica Farmaceutica|
|Data di pubblicazione:||2004|
|Digital Object Identifier (DOI):||10.1002/hlca.200490055|
|Appare nelle tipologie:||01 - Articolo su periodico|